Cho Yong Woo, Lee Jaehwi, Lee Sang Cheon, Huh Kang Moo, Park Kinam
Akina Inc., West Lafayette, IN 47906, USA.
J Control Release. 2004 Jun 18;97(2):249-57. doi: 10.1016/j.jconrel.2004.03.013.
A new experimental method for in vitro release studies of poorly soluble drugs from polymeric micelle systems was developed using a hydrotropic agent, sodium salicylate. It is difficult to maintain a good sink condition for poorly water-soluble drugs, such as paclitaxel (PTX), because of their low aqueous solubility. In this study, a good sink condition for PTX was achieved by using aqueous sodium salicylate solution which solubilized more than 10 times the total amount of PTX incorporated in polymeric micelles. Sodium salicylate at 1 M concentration increased the aqueous PTX solubility by 100 times without destroying the micellar structure of poly(ethylene glycol)-block-poly(phenylalanine) (PEG-b-PPhe) copolymer. PTX was continuously released from PEG-b-PPhe micelles in the hydrotropic release medium. The hydrotropic solution presents a simple method for studying in vitro release behavior of poorly soluble drugs from polymeric micelles in aqueous media.
利用助溶剂水杨酸钠，开发了一种用于研究难溶性药物从聚合物胶束系统中体外释放的新实验方法。由于水溶性低，对于诸如紫杉醇（PTX）等难溶性药物而言，难以维持良好的漏槽条件。在本研究中，通过使用水杨酸钠水溶液实现了PTX的良好漏槽条件，该溶液使掺入聚合物胶束中的PTX总量增溶了10倍以上。1 M浓度的水杨酸钠使PTX的水溶性提高了100倍，同时未破坏聚（乙二醇）-嵌段-聚（苯丙氨酸）（PEG-b-PPhe）共聚物的胶束结构。PTX在助溶释放介质中从PEG-b-PPhe胶束中持续释放。该助溶溶液为研究难溶性药物在水性介质中从聚合物胶束的体外释放行为提供了一种简单方法。
